Solubility: Good solubility in DMSO, with a maximum concentration of up to 3.5 mg/mL (or 6.74 mM, depending on concentration units); Poor solubility in water, <0.1 mg/mL (insoluble).
Stability: Hygroscopic, should be stored under dry conditions.
III. Biological Activity and Pharmacological Effects
ALK Inhibitor: Alectinib Hydrochloride is a potent, selective, and orally available ALK (Anaplastic Lymphoma Kinase) inhibitor with an IC50 value of 1.9 nM and a Kd value of 2.4 nM. It also inhibits certain mutants of ALK, such as ALK F1174L and ALK R1275Q, with IC50 values of 1 nM and 3.5 nM, respectively.
CNS Penetration: Demonstrates effective central nervous system (CNS) penetration, aiding in the treatment of brain tumors.
Antitumor Activity: Shows significant antitumor activity in both in vitro and in vivo studies. For example, it inhibits ALK autophosphorylation in NCI-H2228 cells expressing EML4-ALK and significantly inhibits phosphorylation of STAT3 and AKT. In vivo studies have shown dose-dependent tumor growth inhibition and tumor regression with oral administration of Alectinib Hydrochloride.
